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Submit ReviewMK 0343
说明： GABAA partial agonist; displays subtype selectivity
化学名： 7-Cyclobutyl-3-(2,6-difluorophenyl)-6-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]-1,2,4-triazo[4,3-b]pyridazine
纯度： ≥99% (HPLC)
生物活性 for MK 0343
MK 0343 is a subtype-selective GABAA partial agonist (Ki values are 0.21, 0.22, 0.23 and 0.40 for α3, α1, α5 and α2 respectively); occupies the benzodiazepine site of GABAA receptors. Displays greater agonist efficacy at α3 compared to α1. Exhibits anxiolytic and non-sedating properties in rodent models. Brain penetrant.
技术数据 for MK 0343
| 分子量 | 397.38 |
| 公式 | C19H17F2N7O |
| 储存 | Store at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 233275-76-8 |
| PubChem ID | 22609888 |
| InChI Key | GOIFCXRIFSYPFG-UHFFFAOYSA-N |
| Smiles | FC(C=CC=C3F)=C3C1=NN=C2N1N=C(OCC5=NC=NN5C)C(C4CCC4)=C2 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
产品说明书 for MK 0343
参考文献 for MK 0343
参考文献是支持产品生物活性的出版物。
Atack et al (2011) MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans. J.Psychopharmacol. 25 314 PMID: 20147571
de Haas et al (2008) Pharmacodynamic and pharmacokinetic effects of MK-0343, a GABAA α2,3 subtype-selective agonist, compared to L.pam and placebo in healthy male volunteers. J.Psychopharmacol. 22 24 PMID: 18187530
Atack et al (2010) Benzodiazepine binding site occupancy by the novel GABAA receptor subtype-selective drug 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023) in rats, prima J.Pharmacol.Exp.Ther. 332 17
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关键词: MK 0343, MK 0343 supplier, MK0343, gabaa, subtype-selective, partial, agonists, α3, alpha3, a3, anxiolytics, brain, penetrant, GABAA, Receptors, 4415, Tocris Bioscience
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
GABA Receptors Scientific Review
Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.
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The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.